- 2-GUANIDINO-4-OXO-IMIDAZOLINE DERIVATIVES AS ANTIMALARIAL AGENTS, SYNTHESIS AND METHODS OF USE THEREOF
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The present invention relates to new 2-guanidino-4-oxo-imidazoline derivatives (deoxo-IZ), methods of making these compounds, compositions containing the same, and methods of using the same to prevent, treat, or inhibit malaria in a subject.
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Page/Page column 66; 68
(2012/11/13)
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- Synthesis and antimalarial activity of 2-guanidino-4-oxoimidazoline derivatives
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A series of 2-guanidino-4-oxoimidazoline (deoxo-IZ) derivatives was prepared and showed potent antimalarial activities in rodent and Rhesus models. Compound 8e, the most potent analogues of this series, is the first non-8-aminoqinoline antimalarial that demonstrated radical curative activity in non-human primate by oral route and showed causal prophylactic activity comparable to that of the commonly used clinical drugs in Rhesus monkeys infected with sporozoites of Plasmodium cynomolgi. The metabolic stability and metabolites profile indicated that the new deoxo-IZ derivatives (8) may act as prodrugs of the corresponding IZ (1 and 2) derivatives.
- Liu, Xianjun,Wang, Xihong,Li, Qigui,Kozar, Michael P.,Melendez, Victor,O Neil, Michael T.,Lin, Ai J.
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scheme or table
p. 4523 - 4535
(2011/09/15)
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- PROCESS FOR PRODUCTION OF PYRROLIDINE COMPOUNDS
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A process for the production of compounds represented by the general formula (3) or salts thereof: (3) which comprises reacting a compound represented by the general formula (1): (1) with a compound represented by the general formula (2) or a salt thereof
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Page/Page column 17
(2010/11/25)
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- METHOD OF SEARCHING SUBSTANE HAVING ANTIDIABETIC ACTIVITY
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The present invention provides a screening method of a substance which inhibits binding of a condensed purine derivative to a pancreatic β cell or a treated product of the cell, a substance which inhibits binding of a condensed purine derivative to a protein capable of the condensed purine derivative, and a substance which inhibits the expression or enzymatic activity of a protein capable of a condensed purine derivative, which comprises using the condensed purine derivative and a pancreatic β cell or a treated product of the cell or a protein capable of binding to the condensed purine derivative.
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- Process for producing beta-1, 3-n-acetylglucosamine transferase and n-acetylglucosamine- containing composite saccharide
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The present invention can provide a process for producing a protein having β1,3-N-acetylglucosaminyltransferase activity using a transformant comprising a DNA encoding a protein having β1,3-N-acetylglucosaminyltransferase activity derived from a microorganism belonging to the genus Pasteurella and a process for producing an N-acetylglucosamine-containing complex carbohydrate using a transformant capable of producing a protein having β1,3-N-acetylglucosaminyltransferase activity derived from a microorganism.
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- Process for producing alpha 2,3/ alpha 2,8-sialyltransferase and sialic acid-containing complex sugar
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The present invention can provide a process for producing a protein having α2,3/α2,8-sialyltransferase activity using a transformant comprising a DNA encoding a protein having α2,3/α2,8-sialyltransferase activity derived from a microorganism belonging to the genus Pasteurella and a process for producing a sialic acid-containing complex carbohydrate using a transformant capable of producing a protein having α2,3/α2,8-sialyltransferase activity derived from a microorganism.
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- Beta1, 3-galactose transferase and dna encoding the enzyme
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The present invention provides a protein having β1,3-galactosyltransferase activity, a DNA encoding the protein, a transformant comprising the DNA, a process for producing the protein using the transformant, and a process for producing a galactose-containing complex carbohydrate using the transformant.
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- Process for producing alpha1,4-galactosyltransferase and galactose-containing complex sugar
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The present invention can provide a process for producing a protein having α1.4-galactosyltransferase activity using a transformant comprising a DNA encoding a protein having α1.4-galactosyltransferase activity derived from a microorganism belonging to the genus Pasteurella and a process for producing a galactose-containing complex carbohydrate using a transformant capable of producing a protein having α1,4-galactosyltransferase activity derived from a microorganism.
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- Human CDR-grafted antibody and antibody fragment thereof
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A human CDR-grafted antibody or the antibody fragment thereof which specifically reacts with the extracellular region of human CC chemokine receptor 4 (CCR4) but does not react with a human blood platelet; a human CDR-grafted antibody or the antibody fragment thereof which specifically reacts with the extracellular region of CCR4 and has a cytotoxic activity against a CCR4-expressing cell; and a medicament, a therapeutic agent or a diagnostic agent comprising at least one of the antibodies and the antibody fragments thereof as an active ingredient.
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- Gene recombinant antibody and antibody fragment thereof
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A recombinant antibody or the antibody fragment thereof which specifically reacts with an extracellular domain of human CCR4; a DNA which encodes the recombinant antibody or the antibody fragment thereof; a method for producing the recombinant antibody or the antibody fragment thereof; a method for immunologically detecting CCR4, a method for immunologically detecting a cell which expressed CCR4 on the cell surface, a method for depleting a cell which expresses CCR4 on the cell surface, and a method for inhibiting production of Th2 cytokine, which comprise using the recombinant antibody according or antibody fragment thereof; a therapeutic or diagnostic agent for Th2-mediated immune diseases; and a therapeutic or diagnostic agent for a blood cancer.
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- Azapeptides useful in the treatment of Hepatitis C
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The present invention relates to azapeptide compounds represented by the formula: pharmaceutical compositions containing such compounds, and the use thereof in the treatment of Hepatitis C viral infections.
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- Synthesis and reactions of 9,10-diazatetracyclo-[6.3.0.0.4,110.5.9]undecanes
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The tandem 1,3-dipolar cycloaddition between sydnones and 1,5-cyclooctadiene provides 9,10-diazatetracyclo[6.3.0.0.4,110.5,9]undecanes (the Weintraub reaction) in modest to good yields.
- Gribble, Gordon W.,Hirth, Bradford H.
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p. 719 - 726
(2007/10/03)
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